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Bupropion
Basic Information
Summary
A frequently prescribed atypical antidepressant. Occasionally prescribed as an aid to smoking cessation. May lower seizure threshold in predisposed individuals. Poorly understood mechanism of action, probably an NDRI. Avoid combination with other drugs.
Stimulant
Stimulants excite the nervous system and increase physiological function.
Read more on TripSit Wiki...Habit-forming
These drugs pose a higher risk of causing habit forming behaviour, take particular care with the amount and frequency they are taken.
Read more on TripSit Wiki...Duration
| Parent | |
|---|---|
| Onset | 15-90 minutes |
| Duration | 11-21 hours |
| After-effects | 1-6 hours |
| Metabolites | |
|---|---|
| Onset | 15-90 minutes |
| Duration | 20-37 hours |
| After-effects | 1-6 hours |
General-effects
Mild - moderate increase in motor activity and agitation/excitement
Adverse-effects
Agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation, tremor, dizziness, excessive sweating, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, and auditory disturbance
Overdose-symptoms
Seizure, hallucinations, loss of consciousness, sinus tachycardia, ECG changes, bradycardia, cardiac failure, cardiac arrest, and death
Warning
Bupropion lowers the seizure threshold and can induce seizures when excessive doses are used and/or when combined with CNS stimulants or other drugs that also lower the threshold, such as theophylline, steroids, some tricyclic antidepressants, and alcohol
Chemistry
IUPAC: (±)-2-(tert-Butylamino)-1-(3-chlorophenyl)propan-1-one | Formula: C13H18ClNO | Molecular Mass: 239.74 g/mol
Pharmacology
NDRI (Norepinephrine-Dopamine Reuptake Inhibitor); NDRA (Norepinephrine-Dopamine Releasing Agent); α3β2, α3β4, α4β2, and α7 nACh receptor antagonist
Pharmacokinetics
Protein Binding: 84% (bupropion), 77% [hydroxybupropion (active metabolite)], 42% [threohydrobupropion (active metabolite)] | Metabolism: hepatic, primarily CYP2B6-mediated hydroxylation; both bupropion and hydroxybupropion (active metabolite) are CYP2D6 inhibitors | Excretion: renal (87%; 0.5% unchanged) and faecal (10%)
Legal
Australia: Prescription Only (S4) | Canada: ℞-only | United Kingdom: POM | United States: ℞-only
Aliases
wellbutrin
zyban
amfebutamone
Contradictions
Seizure disorder, current or prior diagnosis of bulimia or anorexia nervosa, abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and anti-epileptic drugs, and MAOIs,
Interactions
No interaction information for Bupropion